Browsing HMS Scholarly Articles by Author "Qi, Jun"

Now showing items 1-5 of 5

    • Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors 

      McKeown, Michael R; Shaw, Daniel L; Fu, Harry; Liu, Shuai; Xu, Xiang; Marineau, Jason J; Huang, Yibo; Zhang, Xiaofeng; Buckley, Dennis L; Kadam, Asha; Zhang, Zijuan; Blacklow, Stephen C; Qi, Jun; Zhang, Wei; Bradner, James E (American Chemical Society, 2014)
      BET bromodomain inhibition has contributed new insights into gene regulation and emerged as a promising therapeutic strategy in cancer. Structural analogy of early methyl-triazolo BET inhibitors has prompted a need for ...

    • Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition 

      Tang, Yujie; Gholamin, Sharareh; Schubert, Simone; Willardson, Minde I.; Lee, Alex; Bandopadhayay, Pratiti; Bergthold, Guillame; Masoud, Sabran; Nguyen, Brian; Vue, Nujsaubnusi; Balansay, Brianna; Yu, Furong; Oh, Sekyung; Woo, Pamelyn; Chen, Spenser; Ponnuswami, Anitha; Monje, Michelle; Atwood, Scott X.; Whitson, Ramon J.; Mitra, Siddhartha; Cheshier, Samuel H.; Qi, Jun; Beroukhim, Rameen; Tang, Jean Y.; Wechsler-Reya, Rob; Oro, Anthony E.; Link, Brian A.; Bradner, James E.; Cho, Yoon-Jae (2014)
      Hedgehog signaling drives oncogenesis in several cancers and strategies targeting this pathway have been developed, most notably through inhibition of Smoothened. However, resistance to Smoothened inhibitors occurs via ...

    • Genome-wide determination of drug localization 

      Anders, Lars; Guenther, Matthew G.; Qi, Jun; Fan, Zi Peng; Marineau, Jason J.; Rahl, Peter B.; Lovén, Jakob; Sigova, Alla A.; Smith, William B.; Lee, Tong Ihn; Bradner, James E.; Young, Richard A. (2014)
      A vast number of small-molecule ligands, including therapeutic drugs under development and in clinical use, elicit their effects by binding specific proteins associated with the genome. An ability to map the direct ...

    • An oncogenic MYB feedback loop drives alternate cell fates in adenoid cystic carcinoma 

      Drier, Yotam; Cotton, Matthew J.; Williamson, Kaylyn E.; Gillespie, Shawn M.; Ryan, Russell J.H.; Kluk, Michael J.; Carey, Christopher D.; Rodig, Scott J.; Sholl, Lynette M; Afrogheh, Amir H.; Faquin, William C.; Queimado, Lurdes; Qi, Jun; Wick, Michael J.; El-Naggar, Adel K.; Bradner, James E.; Moskaluk, Christopher A.; Aster, Jon C.; Knoechel, Birgit; Bernstein, Bradley E. (2016)
      Translocation events are frequent in cancer and may create chimeric fusions or ‘regulatory rearrangements’ that drive oncogene overexpression. Here we identify super-enhancer translocations that drive overexpression of the ...

    • Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement 

      Yi, Joanna S.; Federation, Alexander J.; Qi, Jun; Dhe-Paganon, Sirano; Hadler, Michael; Xu, Xiang; St. Pierre, Roodolph; Varca, Anthony C.; Wu, Lei; Marineau, Jason J.; Smith, William B.; Souza, Amanda; Chory, Emma J.; Armstrong, Scott A.; Bradner, James E. (American Chemical Society, 2014)
      The DOT1L lysine methyltransferase has emerged as a validated therapeutic target in MLL-rearranged (MLLr) acute leukemias. Although S-adenosylmethionine competitive inhibitors have demonstrated pharmacological proof-of-principle ...